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Compound Detail

CHEMBL36654

ROEMERINE
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CN1CCc2cc3c(c4c2C1Cc1ccccc1-4)OCO3

Basic Information

ChEMBL ID CHEMBL36654
Name ROEMERINE
Phase Preclinical
Structure Type MOL
InChI Key JCTYWRARKVGOBK-UHFFFAOYSA-N
9
Targets
16
Activities
3
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

279.3
MW (Da)
3.17
ALogP
3
HBA
0
HBD
21.7
PSA (Ų)
0.74
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C18H17NO2
MW 279.34
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness 1.46

Activity Summary

IC50 7 meas. best 5.78
EC50 5 meas. best 7.1
Ki 4 meas. best 7.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein RecA
CHEMBL1741171
EC50 7.1 7.1 79.7 1
D(2) dopamine receptor
CHEMBL339
Ki 7.08 7.08 83.2 2
Plasmodium falciparum
CHEMBL364
EC50 7.03 6.99 93.1 2
D(1A) dopamine receptor
CHEMBL265
Ki 6.49 6.455 324.3 2
Unchecked
CHEMBL612545
IC50 5.78 5.575 1660.0 4
Apoptotic protease-activating factor 1
CHEMBL1795093
IC50 4.99 4.99 10200.0 1
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
IC50 4.82 4.82 15000.0 1
RNA-binding protein pos-1
CHEMBL1293304
EC50 4.77 4.77 16837.0 1
Zinc finger protein mex-5
CHEMBL1293319
EC50 4.67 4.67 21456.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein RecA EC50 = 79.7 nM 7.1 PUBCHEM_BIOASSAY: Fluorescence Cell-Free Homogeneous Dose Retest to Identify Inh... -
D(2) dopamine receptor Ki = 83.18 nM 7.08 Displacement of [3H]-raclopride from D2 receptor of Wistar rat striatal membrane... 23886690
D(2) dopamine receptor Ki = 84.0 nM 7.08 Displacement of [3H]-raclopride from D2 receptor of Wistar rat striatal membrane... 23886690
Plasmodium falciparum EC50 = 93.1 nM 7.03 NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferati... 18579783
Plasmodium falciparum EC50 = 111.5 nM 6.95 NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation ... 18579783
D(1A) dopamine receptor Ki = 324.34 nM 6.49 Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes ... 23886690
D(1A) dopamine receptor Ki = 377.0 nM 6.42 Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes ... 23886690
Unchecked IC50 = 1660.0 nM 5.78 PUBCHEM_BIOASSAY: High Throughput Screening Assay used to Identify Novel Compoun... -
Unchecked IC50 = 2350.0 nM 5.63 PUBCHEM_BIOASSAY: A High Throughput Confirmatory Assay used to Identify Novel Co... -
Unchecked IC50 = 2730.0 nM 5.56 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 using a LZ-... -
Unchecked IC50 = 4695.0 nM 5.33 PubChem BioAssay. TRFRET-based biochemical high throughput dose response assay t... -
Apoptotic protease-activating factor 1 IC50 = 10200.0 nM 4.99 PUBCHEM_BIOASSAY: Dose response confirmation of uHTS hits for Apaf-1 in a Fluore... -
Dual specificity tyrosine-phosphorylation-regulated kinase 1A IC50 = 15000.0 nM 4.82 Inhibition of DYRK1A (unknown origin) 30243157
RNA-binding protein pos-1 EC50 = 16837.0 nM 4.77 PUBCHEM_BIOASSAY: Fluorescent Polarization Homogeneous Dose Response HTS to Iden... -
Zinc finger protein mex-5 EC50 = 21456.0 nM 4.67 PUBCHEM_BIOASSAY: Fluorescent Polarization Homogeneous Dose Response HTS to Iden... -

Literature References

PubMed DOI Target Context # Activities
18579783 10.1073/pnas.0802982105 Plasmodium falciparum 2
23886690 10.1016/j.bmcl.2013.06.078 D(2) dopamine receptor 2
23886690 10.1016/j.bmcl.2013.06.078 D(1A) dopamine receptor 2
- 10.1016/0960-894X(95)00250-W Protein tyrosine phosphatase receptor type C-associated protein 1
18579783 10.1073/pnas.0802982105 Unchecked 1
18579783 10.1073/pnas.0802982105 Huh-7 1
23886690 10.1016/j.bmcl.2013.06.078 Unchecked 1
30243157 10.1016/j.ejmech.2018.08.093 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1

Data from ChEMBL 36 via Core Engine